US2019350995A1PendingUtilityA1
Therapeutic composition derived from anthostema senegalense
Est. expiryOct 21, 2036(~10.2 yrs left)· nominal 20-yr term from priority
Inventors:Aliou Mamadou Balde
A61P 31/18A61K 36/47A61K 2236/51A61K 31/56A61K 2236/17A23L 33/11A61K 2236/33C07J 63/008
19
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Claims
Abstract
The present invention relates to a chemical composition characterized in that it comprises:—the molecule A or a physiologically acceptable salt thereof, and/or:—the molecule B or a physiologically acceptable salt thereof, said molecule A having the following formula: and the molecule B having the following formula: the molecule A or a physiologically acceptable salt thereof being biologically active and stimulating immune activity, the molecule B or a physiologically acceptable salt thereof being biologically active and stimulating immune activity.
Claims
exact text as granted — not AI-modified1 . A chemical composition comprising at least one selected from the group consisting of:
a molecule A or one of physiologically acceptable salts thereof;
and
a molecule B or one of physiologically acceptable salts thereof,
the molecule A having the following formula:
and said molecule B having the following formula:
wherein the molecule A or one of the physiologically acceptable salts thereof is biologically active and is a stimulator of immune activity;
wherein the molecule B or one of the physiologically acceptable salts thereof is biologically active and is a stimulator of immune activity.
2 . The chemical composition according to claim 1 , wherein the molecule A has at least one selected from the group consisting of:
at position 16, as a substitute for the carbonyl function ═O, either an —OH, or an aldehyde carbonyl group —RCOH, or a ketone —R1-CO—R2, or an ester —R—COO—R′, or an amide of the type —R—C(═O)NH2; and at position 3, a glycosylation or esterification in the form of —OR, where “R” is either a feruloyl or caffeoyl group, or a sugar or an amide.
3 . The chemical composition according to claim 1 , wherein the molecule A is conjugated with at least one selected from the group consisting of amino acids, quaternary ammonium salts, glycosides, hemiphtalates and carbamates.
4 . The chemical composition according to claim 1 , wherein the molecule B has, at position 28, an esterification of an amide or a sugar.
5 . The chemical composition according to claim 1 , wherein the composition further comprises at least one of the following molecules or one of physiologically acceptable salts thereof, or one of possible combinations of the following molecules, the one or more molecule(s) being selected from the following list:
molecule C having the formula:
wherein “n” is comprised between 8 and 26;
molecule D having the formula:
molecule E having the formula:
molecule F having the formula:
molecule G having the formula:
molecule H having the formula:
molecule I having the formula:
wherein “n” is comprised between 14 and 26;
molecule J having the formula:
6 . The chemical composition according to claim 1 , wherein each of the molecules A, B, and each of the physiologically acceptable salts thereof is of synthetic origin and derived from a chemical synthesis in the laboratory or from a hemi-synthesis.
7 . The chemical composition according to claim 1 , wherein each of the molecules A, B and each of the physiologically acceptable salts thereof is of natural origin and derived from a plant extract of Anthostema senegalense.
8 . The chemical composition according to claim 7 , wherein the plant extract of Anthostema senegalense consists of a polar extract, that is aqueous, alcoholic or hydro-alcoholic or an apolar or non-polar extract or a mother tincture of Anthostema senegalense with an ethanol content of 70% V/V.
9 . The chemical composition according to claim 8 , wherein the plant extract is obtained from the trunk/stem bark, in particular dried bark, of Anthostema senegalense.
10 . The chemical composition according to claim 1 , which is in the form of a medicament or a food-dietary supplement.
11 . A pharmaceutical composition comprising the chemical composition according to claim 1 , which is formulated for the treatment of at least one selected from the group consisting of HIV infection type 1, HIV infection type type 2, AIDS, and clinical manifestations that accompany AIDS.
12 . The pharmaceutical composition according to claim 11 , which is in an oral galenic form.
13 . The pharmaceutical composition according to claim 11 , which is in an oral galenic form of microspheres produced by a method of extrusion and spheronisation, tablets, soft capsules, granules, gel capsules, powders, ampoules, syrups or decoctions.
14 . An isolation method for isolating by extraction, identification and selection of the one or more biologically active molecule(s) of the chemical composition according to claim 1 , the method comprising:
drying a part of the Anthostema senegalense plant to obtain a dried part of the plant; preparing a plant extract from the dried part of the plant, by extraction with an apolar or polar solvent or by maceration, infusion, decoction, percolation, digestion or leaching; concentrating the plant extract is concentrated under vacuum; separating molecules of the plant extract by chromatography; carrying out in vitro testing is on the biological activity of the molecules against an HIV-type viral pathogen according to the method of E de Clercq; selecting and isolating molecules having a selectivity index against the pathogen ≥50 and a 50% cytotoxic concentration CC 50 ≥45 μg/mL; identifying the one or more molecule(s) that have been separated, selected and isolated by means of nuclear magnetic resonance and mass spectrometry.
15 . The method according to claim 14 , wherein:
the part of the Anthostema senegalense plant which is dried consists of the bark of the trunk/stem, or the bark of the roots, or the leaves or the fruits; the plant extract is prepared by percolation with CHCl3 in order to obtain an apolar plant extract; after concentration under vacuum, the molecules of the plant extract are separated by repeated column chromatography and thin layer chromatography.
16 . The method according to claim 15 , wherein the molecules of the apolar plant extract are separated by repeated column chromatography, using as stationary phase a polar silica gel and, as mobile phase, an apolar eluent constituted of a gradient of CHCl 3 in hexane.
17 . The chemical composition according to claim 2 , wherein the molecule A is conjugated with at least one selected from the group consisting of amino acids, quaternary ammonium salts, glycosides, hemiphtalates and carbamates.
18 . The chemical composition according to claim 17 , wherein the molecule B has, at position 28, an esterification of an amide or a sugar.
19 . The chemical composition according to claim 2 , wherein the molecule B has, at position 28, an esterification of an amide or a sugar.
20 . The chemical composition according to claim 3 , wherein the molecule B has, at position 28, an esterification of an amide or a sugar.Join the waitlist — get patent alerts
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